Monocarbams are a class of synthetic monocyclic beta-lactam antibacterial agents which have as their salient feature, a substituted sulfonylaminocarbonyl activating group at the N−1 position. The early studies in this area were conducted by workers at the Squibb Institute for Medical Research, Cimarusti, C. M. & R. B. Sykes: Monocyclic β-lactam antibiotics. Med. Res. Rev. 4: 17˜20, 1984. Monocarbams have also been previously discussed in EP 0281289, published Sep. 7, 1988. These and all documents cited herein are fully incorporated in their entirety by reference herein.
Although not limiting to the present invention, it is believed that monocarbams of the present invention exploit the iron uptake mechanism in bacteria through the use of siderphore-monobactam and siderphore-monocarbam conjugates. Barbachyn, M. R., Tuominen, T. C.: Synthesis And Structure-Activity Relationships of Monocarbams Leading to U-78608. Journal of Antibiotics Vol. XLIII No. 9: 1199-1203, 1990. Thus, at least in general terms, the activity and mechanism of action of monocarbams are generally known, although the present invention is not bound or limited by any theory.
There is a continuing need for new antibiotics, such as monocarbams, in response to the increasing emergence of resistant organisms and to improve safety, among other reasons.